nilotinib (Rx)

Brand and Other Names:Tasigna
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 150mg
  • 200mg

Chronic Myeloid Leukemia

Newly diagnosed Philadelphia chromosome positive (Ph+) chronic phase (CP) chronic myeloid leukemia (CML)

  • Indicated for initial treatment of newly diagnosed Ph+ CML-CP
  • 300 mg PO q12hr

Resistant or intolerant

  • Indicated for treatment of CP and accelerated phase (AP) Ph+ CML in patients resistant to or intolerant to prior therapy that included imatinib
  • 400 mg PO q12hr

Dosage Modifications

Neutropenia and thrombocytopenia

  • Adults with newly diagnosed Ph+ CP-CML or resistant or intolerant CP and AP Ph+ CML
  • Absolute neutrophil count (ANC) <1 x 109/L or platelet <50 x 109/L: Stop therapy and monitor blood cell counts
  • Within 2 weeks of recovery: Resume original dose if ANC >1 x 109/L & platelet >50 x 109/L
  • If levels remain low for >2 weeks: Reduce to 400 mg qDay

QT Prolongation (QTc >480 msec)

  • Withhold and analyze serum potassium and magnesium; correct any abnormalities with electrolyte supplementation
  • Review concomitant medications for additive effects or interactions that increase nilotinib systemic exposure
  • Resume within 2 weeks at prior dose if QTc returns to <450 msec and to within 20 msec of baseline
  • If QTc is between 450-480 msec after 2 weeks, reduce to 400 mg qDay
  • Discontinue if QTc returns to >480 msec despite dose reduction
  • Repeat ECG ~7 days after any dose adjustment

Moderate or severe nonhematologic toxicity

  • Withhold until toxicity resolves
  • Newly diagnosed Ph+ CML-CP
    • Resume at 400 mg qDay if previous dose was 300 mg BID; discontinue treatment if prior dose was 400 mg qDay
    • If clinically appropriate, consider re-escalate dose to 300 mg BID
  • Resistant or intolerant Ph+ CML-CP and CML-AP
    • Resume at 400 mg qDay if previous dose was 400 mg BID; discontinue treatment if prior dose was 400 mg qDay
    • If clinically appropriate, consider re-escalate dose to 400 mg BID

Elevated serum lipase or amylase Grade ≥3

  • Withhold and monitor serum lipase or amylase
  • Resume at 400 mg qDay if serum lipase or amylase returns to Grade ≤1

Elevated bilirubin or ALT/AST Grade ≥3

  • Withhold and monitor bilirubin
  • Resume at 400 mg qDay if serum bilirubin returns to Grade ≤1

Consider discontinuation of treatment after a sustained molecular response

  • Monitor BCR-ABL transcript levels and complete blood count (CBC) with differential in patients who have discontinued therapy monthly for 1 year, then q6Weeks for the second year, and q12Weeks thereafter
  • Newly diagnosed Ph+ CML-CP
    • Treatment with nilotinib for at least 3 years
    • Maintain a molecular response of at least MR4 (corresponding to = BCR-ABL/ABL ≤0.01% IS) for 1 year prior to discontinuation of therapy
    • Achieved an MR4.5 for the last assessment taken immediately prior to discontinuation of therapy
    • Been confirmed to express the typical BCR-ABL transcripts (e13a2/b2a2 or e14a2/b3a2)
    • No history of accelerated phase or blast crisis
    • No history of prior attempts of treatment-free remission discontinuation that resulted in relapse
  • Patients with Ph+ CML-CP that are resistant or intolerant to treatment with imatinib
    • Treatment with nilotinib for at least 3 years
    • Previously treated with imatinib only prior to treatment with nilotinib
    • Achieved a molecular response (MR) of MR.4.5 (corresponding to = BCR-ABL/ABL ≤0.0032% IS)
    • Sustained an MR4.5 for a minimum of one year immediately prior to discontinuation of therapy
    • Been confirmed to express the typical BCR-ABL transcripts (e13a2/b2a2 or e14a2/b3a2)
    • No history of accelerated phase or blast crisis
    • No history of prior attempts of treatment-free remission discontinuation that resulted in relapse

Reinitiating treatment if MR lost after discontinuing therapy

  • Newly diagnosed patients
    • Patients who lose major molecular response (MMR) must reinitiate treatment within 4 weeks at the dose level prior to discontinuing treatment
    • Monitor BCR-ABL transcript levels monthly until MMR is re-established and q12Weeks thereafter
  • Resistant or intolerant Ph+ CML (chronic phase or accelerated phase) H5
    • Patients resistant or intolerant to prior treatment that included imatinib with confirmed loss of MR4 (2 consecutive measures separated by at least 4 weeks showing loss of MR4) or loss of MMR must reinitiate treatment within 4 weeks at dose level before discontinuing therapy
    • Monitor BCR-ABL transcript levels monthly until previous major molecular response or MR 4 is re-established and q12Weeks thereafter

Coadministration with strong CYP3A4 inhibitors

  • Avoid coadministration
  • Should treatment of strong CYP3A4 inhibitors be required, interrupt nilotinib therapy
  • If coadministration is unavoidable, reduce nilotinib dose to 300 mg/day in patients with resistant or intolerant Ph+ CML or to 200 mg/day with newly diagnosed Ph+ CML-CP; closely monitor for QT prolongation
  • No clinical data are available with this dose adjustment in patients receiving strong CYP3A4 inhibitors
  • If strong inhibitor is discontinued, allow a washout period before adjusting nilotinib dose upward to indicated dose

Coadministration with strong CYP3A4 inducers

  • Avoid coadministration
  • Based on nonlinear pharmacokinetic profile of nilotinib, increasing the dose is unlikely to compensate for loss of nilotinib systemic exposure

Renal impairment

  • Clinical studies have not been performed in patients with impaired renal function
  • Since nilotinib and its metabolites are not renally excreted, a decrease in total body clearance is not anticipated in patients with renal impairment

Hepatic impairment

  • Newly diagnosed Ph+ CML (chronic phase at 300 mg BID)
    • Mild-to-severe (Child-Pugh A to C): Reduce to 200 mg BID; may increase to 300 mg BID based on tolerability
  • Resistant or intolerant Ph+ CML-CP or -AP
    • Mild or moderate (Child-Pugh A to B): Reduce to 300 mg BID; may increase to 400 mg BID based on tolerability
    • Severe (Child-Pugh C): Reduce to 200 mg BID; may increase to 300 mg BID, and then 400 mg BID based on tolerability

Dosage Forms & Strengths

capsule

  • 50mg
  • 150mg
  • 200mg

Chronic Myeloid Leukemia

Indicated for initial treatment of newly diagnosed Philadelphia chromosome positive chronic phase chronic myeloid leukemia (Ph+ CP-CML) in children aged ≥1 year and adolescents

Also, indicated for children and adolescents aged ≥1 year with CP and accelerated phase (AP) Ph+ CML resistant or intolerant to prior tyrosine-kinase inhibitor (TKI) therapy

230 mg/m2 PO BID, round to the nearest 50-mg dose; not to exceed 400 mg/dose

Continue until disease progression or unacceptable toxicity

Dosing based on body surface area (BSA)

  • ≤0.32 m2: 50 mg per dose; total daily dose (TDD): 100 mg
  • 0.33–0.54 m2: 100 mg per dose; TDD: 200 mg
  • 0.55–0.76 m2: 150 mg per dose; TDD: 300 mg
  • 0.77–0.97 m2: 200 mg per dose; TDD: 400 mg
  • 0.98–1.19 m2: 250 mg per dose; TDD: 500 mg
  • 1.2–1.41 m2: 300 mg per dose; TDD: 600 mg
  • 1.42–1.63 m2: 350 mg per dose; TDD: 700 mg
  • ≥1.64 m2: 400 mg per dose; TDD: 800 mg

Dosage Modifications

Neutropenia and thrombocytopenia

  • Stop nilotinib and monitor blood cell counts
  • Resume within 2 weeks to original dose if ANC >1.5 x 109/L and/or platelets >75 x 109/L
  • If ANC remains low for >2 weeks: Reduce dose to 230 mg/m2 qDay
  • If event occurs after dose reduction, consider discontinuing treatment

QT Prolongation (QTc >480 msec)

  • Withhold and analyze serum potassium and magnesium; correct any abnormalities with electrolyte supplementation
  • Review concomitant medications for additive effects or interactions that increase nilotinib systemic exposure
  • Resume within 2 weeks at prior dose if QTc returns to <450 msec and to within 20 msec of baseline
  • If QTc is between 450-480 msec after 2 weeks, reduce dose to 230 mg/m² qDay
  • Discontinue if QTc returns to >480 msec despite dose reduction
  • Repeat ECG ~7 days after any dose adjustment

Moderate or severe nonhematologic toxicity

  • Interrupt therapy until toxicity has resolved
  • Resume treatment at 230 mg/m2 qDay if previous dose was 230 mg/m2 BID; discontinue treatment if prior dose was 230 mg/m2 qDay
  • If clinically appropriate, consider re-escalating dose to 230 mg/m2 BID

Elevated serum lipase or amylase Grade ≥3

  • Interrupt nilotinib until the event returns to Grade ≤1
  • Resume at 230 mg/m2 qDay if prior dose was 230 mg/m2 BID; discontinue treatment if prior dose was 230 mg/m2 qDay

Elevated bilirubin or AST/ALT Grade ≥3

  • Interrupt therapy until the event returns to Grade ≤1
  • Resume at 230 mg/m2 qDay if prior dose was 230 mg/m2 BID; discontinue treatment if prior dose was 230 mg/m2 qDay, and recovery to Grade ≤1 takes >28 days

Consider discontinuation of treatment after a sustained molecular response

  • Monitor BCR-ABL transcript levels and complete blood count (CBC) with differential in patients who have discontinued therapy monthly for 1 year, then q6Weeks for the second year, and q12Weeks thereafter
  • Newly diagnosed Ph+ CML-CP
    • Treatment for at least 3 years
    • Maintain a molecular response (MR) of at least MR4 (corresponding to = BCR-ABL/ABL ≤0.01% IS) for 1 year before discontinuing therapy
    • Achieved an MR4.5 for the last assessment taken immediately before discontinuing therapy
    • Been confirmed to express the typical BCR-ABL transcripts (e13a2/b2a2 or e14a2/b3a2)
    • No history of AP or blast crisis
    • No history of prior attempts of treatment-free remission discontinuation that resulted in relapse
  • Ph+ CML-CP that are resistant or intolerant to treatment with imatinib who have achieved a sustained MR (MR4.5)
    • Treatment for at least 3 years
    • Previously treated with imatinib only prior to nilotinib
    • Achieved a molecular response of MR.4.5 (corresponding to = BCR-ABL/ABL ≤0.0032% IS)
    • Sustained an MR4.5 for a minimum of 1 year immediately prior to discontinuation of therapy
    • Been confirmed to express the typical BCR-ABL transcripts (e13a2/b2a2 or e14a2/b3a2)
    • No history of AP or blast crisis
    • No history of prior attempts of treatment-free remission discontinuation that resulted in relapse

Reinitiating treatment if MR lost after discontinuing therapy

  • Newly diagnosed patients
    • Patients who lose major molecular response (MMR) must reinitiate treatment within 4 weeks at dose level before discontinuing treatment
    • Monitor BCR-ABL transcript levels monthly until MMR is re-established and q12Weeks thereafter
  • Resistant or intolerant Ph+ CML (CP or AP)
    • Patients resistant or intolerant to prior treatment that included imatinib with confirmed loss of MR4 (2 consecutive measures separated by at least 4 weeks showing loss of MR4) or loss of MMR must reinitiate treatment within 4 weeks at dose level prior to discontinuation of therapy
    • Monitor BCR-ABL transcript levels monthly until previous MMR or MR 4 is re-established and q12Weeks thereafter

Coadministration with strong CYP3A4 inhibitors

  • Avoid coadministration
  • Should treatment of strong CYP3A4 inhibitors be required, interrupt nilotinib therapy
  • No clinical data are available with this dose adjustment in patients receiving strong CYP3A4 inhibitors
  • If strong inhibitor is discontinued, allow a washout period before adjusting nilotinib dose upward to indicated dose

Coadministration with strong CYP3A4 inducers

  • Avoid coadministration
  • Based on nonlinear pharmacokinetic profile of nilotinib, increasing the dose is unlikely to compensate for loss of nilotinib systemic exposure
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Interactions

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and nilotinib

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            Adverse Effects

            >10%

            Rash (33%)

            Headache (31%)

            Nausea (31%)

            Pruritus (29%)

            Fatigue (28%)

            Pyrexia (24%)

            Diarrhea (22%)

            Constipation (21%)

            Vomiting (21%)

            Arthralgia (18%)

            Cough (17%)

            Extremity pain (16%)

            Asthenia (14%)

            Muscle spasms (14%)

            Myalgia (14%)

            Abdominal pain (13%)

            Bone pain (13%)

            Back pain (12%)

            Dyspnea (11%)

            Nasopharyngitis (11%)

            Peripheral edema (11%)

            1-10% (selected)

            Dizziness

            Insomnia

            Paresthesia

            QT interval prolongation

            HTN

            Palpitations

            QT interval prolongation

            Hyperglycemia

            Hyperkalemia

            Hypomagnesemia

            Neutropenia

            Pancytopenia

            <1%

            Peripheral arterial occlusive disease

            Tumor lysis syndrome

            Aortic valve sclerosis

            Abscess

            Amnesia

            Dehydration

            Postmarketing Reports

            Infections: Hepatitis B virus reactivation

            Sepsis, subcutaneous abscess, anal abscess, furuncle, tinea pedis

            Thrombotic microangiopathy

            Nervous system disorders: Facial paralysis

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            Warnings

            Black Box Warnings

            QT prolongation

            • Prolongs QT interval; sudden death reported
            • Do not use in patients with hypokalemia, hypomagnesemia, or long QT syndrome
            • Must correct hypokalemia or hypomagnesemia before initiating therapy
            • Monitor potassium and magnesium periodically
            • Avoid drugs known to prolong QT and strong CYP3A4 inhibitors
            • Reduced dose with hepatic impairment
            • Monitor QTc through electrocardiograms (ECGs) at baseline, 7 days after initiation, and periodically thereafter following any dose adjustments
            • Take on empty stomach; avoid food 2 hr before and 1 hr after taking dose

            Contraindications

            Long QT syndrome, hypokalemia, hypomagnesemia

            Cautions

            Grade 3/4 thrombocytopenia, neutropenia and anemia may occur; perform complete blood cell counts (CBC) every 2 weeks for first 2 months and then monthly thereafter, or as clinically indicated; myelosuppression was generally reversible and usually managed by withholding drug temporarily or dose reduction

            Sudden deaths reported; ventricular repolarization abnormalities may have contributed to their occurrence; evaluate cardiovascular status and monitor/manage cardiovascular risk factors during therapy

            QT interval reported; significant prolongation of the QT interval may occur when drug is inappropriately taken with food; avoid taking with food; prolongation of the QT interval can result in torsade de pointes, which may result in syncope, seizure, and/or death

            May cause hypophosphatemia, hypokalemia, hyperkalemia, hypocalcemia, and hyponatremia; correct hypokalemia or hypomagnesemia before administration; monitor periodically during therapy

            Cardiovascular events (eg, ischemic heart disease, peripheral arterial occlusive disease, ischemic cerebrovascular events) reported in patients with newly diagnosed Ph+ CML; evaluate cardiovascular status, monitor cardiovascular risk factors, and manage during therapy

            Use caution in history of pancreatitis; monitor serum lipase monthly or as clinically indicated; in case lipase elevations are accompanied by abdominal symptoms, interrupt doses and consider appropriate diagnostics to exclude pancreatitis

            Use caution in hepatic impairment; monitor hepatic function tests (HFTs) monthly or as clinically indicated; reduce dose and monitor QT interval

            May result in elevations in bilirubin, AST/ALT, and alkaline phosphatase; Grade 3-4 elevations of bilirubin, AST, and ALT were reported at higher frequency in pediatric than in adult patients; monitor HFTs monthly or as clinically indicated

            Tumor lysis syndrome cases reported in patients with resistant or intolerant CML; maintain adequate hydration and correct uric acid levels prior to initiating therapy

            Total gastrectomy may reduce nilotinib systemic exposure; perform more frequent follow-up of these patients; if necessary, consider dose increase or alternative therapy

            Hemorrhage from any site may occur; advise patients to report signs and symptoms of bleeding and medically manage as needed

            Monitor for signs of severe fluid retention (eg, unexpected rapid weight gain, swelling) and for symptoms of respiratory or cardiac compromise (eg, shortness of breath) during treatment; evaluate etiology and treat patients accordingly

            May cause fetal harm

            Growth retardation reported in pediatric patients with Ph+ CML-CP; growth deceleration was more pronounced in children aged <12 years at baseline; monitor growth and development in pediatric patients

            Monitoring BCR-ABL transcript levels

            • Monitoring transcript levels in patients who discontinued therapy
            • Monitor BCR-ABL transcript levels in patients eligible for treatment discontinuation using an FDA authorized test validated to measure MR levels with a sensitivity of at least MR4.5 (BCR-ABL/ABL ≤ 0.0032% IS)
            • In patients who discontinue therapy, assess BCR-ABL transcript levels monthly for 1 year, then every 6 weeks for the second year and every 12 weeks thereafter during treatment discontinuation
            • For patients who fail to achieve MMR after 3 months of treatment reinitiation, perform BCR-ABL kinase domain mutation testing
            • Monitoring of BCR-ABL transcript levels in patients who have reinitiated therapy after loss of molecular response
            • Monitor CBC and BCR-ABL transcripts in patients who reinitiate treatment with Tasigna due to loss of MR quantitation every 4 weeks until a major molecular response is re-established, then every 12 weeks

            Drug interaction overview

            • Substrate of CYP3A4
            • Clinical significance unknown: Competitive inhibitor of CYP2C8, CYP2D6, and is an inducer of CYP2B6 and CYP2C8; inhibitor of UGT1A1 and P-gp
            Strong CYP3A4 inhibitors
            • Avoid coadministration; if unable to avoid, decrease dose and monitor for QT prolongation
            • Strong CYP3A4 inhibitors may increase concentrations and adverse reactions of nilotinib
            Strong CYP3A4 inducers
            • Avoid coadministration
            • Strong CYP3A4 inducers may decrease concentrations and adverse reactions of nilotinib
            Proton pump inhibitors (PPIs)
            • Avoid coadministration
            • PPIs decrease nilotinib concentrations and efficacy
            • As an alternative, use H2-blockers ~10 hr before or ~2 hr after nilotinib, or use antacids ~2 hr before or ~2 hr after nilotinib
            Drugs that prolong QT interval
            • Avoid coadministration
            • Coadministration with drugs that prolong QT interval may potentiate the QT-prolonging effects of nilotinib
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            Pregnancy & Lactation

            Pregnancy

            No available data in pregnant women to inform the drug-associated risk; in animal reproduction studies, administration of nilotinib to pregnant rats and rabbits during organogenesis caused adverse developmental outcomes including embryo-fetal lethality, fetal effects, and fetal variations in rats and rabbits at maternal exposures (AUC) approximately 2 and 0.5 times, respectively, exposures in patients at recommended dose; advise pregnant women of potential risk to fetus

            Pregnancy test

            • Females of reproductive potential should have a pregnancy test prior to starting treatment

            Contraception

            • Based on animal studies, drug can cause fetal harm when administered to a pregnant woman; advise females of reproductive potential to use effective contraception during treatment with drug and for at least 14 days after the last dose

            Infertility

            • The risk of infertility in females or males of reproductive potential has not been studied in humans; in studies in rats and rabbits, the fertility in males and females was not affected

            Lactation

            No data are available regarding the presence of nilotinib or its metabolites in human milk or its effects on a breastfed child or on milk production

            However, nilotinib is present in the milk of lactating rats

            Owing to the potential for serious adverse reactions in a nursing child, advise lactating women not to breastfeed during treatment and for at least 14 days after the last dose

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Selectively binds with high affinity to ATP-binding site of BCR-ABL kinase inhibiting cell proliferation in cell lines and in primary Ph+ CML leukemia cells

            Active against imatinib-resistant mutant forms of Bcr-Abl

            Inhibits PDGFR and c-Kit kinase

            Absorption

            Peak plasma concentration: 1,540 ng/ml (300 mg BID)

            AUC: 13,337 ng·hr/ml (300 mg BID)

            Peak plasma time: 3 hr

            Distribution

            Protein Bound: 98%

            Blood-to-serum ratio: 0.68

            Metabolism

            Oxidation and hydroxylation by liver CYP3A4

            Enzymes Inhibited: CYP3A4, CYP2C8, CYP2C9, CYP2D6, UGT1A1

            Enzymes Induced CYP2B6, CYP2C8, CYP2C9

            Elimination

            Half-life: ~17 hr

            Clearance: ~29 L/hr

            Excretion: Feces 93%

            Pharmacogenomics

            Confirmed BCR-ABL transcripts

            • Tyrosine kinase inhibitors (TKIs) inhibit activity of BCR-ABL fusion protein, resulting in both hematologic response (ie, normal cell counts in the peripheral blood and normal bone marrow morphology), as well as cytogenetic response (ie, disappearance or reduction of the Philadelphia [Ph] chromosome)
            • NCCN clinical practice guidelines recommends TKIs in CML with confirmed BCR-ABL transcripts in bone marrow or evidence of translocation on cytogenetics

            UGT1A1 and increased bilirubin

            • Polymorphisms of UGT1A1 and its potential association with hyperbilirubinemia during nilotinib treatment have been studied
            • The (TA)7/(TA)7 genotype was associated with a statistically significant increase in the risk of hyperbilirubinemia relative to the (TA)6/(TA)6 and (TA)6/(TA)7 genotypes
            • However, the largest increases in bilirubin were observed in the (TA)7/(TA)7 genotype (UGT1A1*28) patients during nilotinib treatment

            Genetic testing laboratories

            • The following companies currently offer FISH and/or transcript quantification testing for BCR-ABL
            • Asuragen (http://www.asuragen.com/)
            • Dako (http://www.dakousa.com/)
            • Invitrogen (http://www.invitrogen.com/)
            • Ipsogen (http://www.ipsogen.com)
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            Administration

            Oral Administration

            Take twice daily at ~12-hr intervals (unless dosage modification required)

            Administer on empty stomach; do not consume food for at least 2 before the dose and for at least 1 hr after the dose is taken

            Swallow capsule whole with water

            If unable to swallow capsules, capsule contents may be dispersed in 1 teaspoon of applesauce; take mixture immediately (within 15 minutes) and do not be stored for future use

            Missed dose

            • If a dose is missed, take the next dose as scheduled
            • Do not double dose to make up for missed doses

            Storage

            Tablets: Store at room temperature between 68-77°F (20-25°C)

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            Images

            BRAND FORM. UNIT PRICE PILL IMAGE
            Tasigna oral
            -
            200 mg capsule

            Copyright © 2010 First DataBank, Inc.

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            Patient Handout

            Patient Education
            nilotinib oral

            NILOTINIB - ORAL

            (nye-LOE-ti-nib)

            COMMON BRAND NAME(S): Tasigna

            WARNING: This drug can rarely cause serious (possibly fatal) irregular heartbeats (QT prolongation). Nilotinib should not be used in people with low blood levels of certain minerals (potassium, magnesium) or a certain heart problem (long QT syndrome). To lower your risk, your doctor will order certain blood tests (potassium/magnesium levels, liver function tests) before and during treatment with nilotinib. You should have a heart test (EKG) before starting nilotinib. The EKG should be repeated 7 days after your first dose, when your dose is changed, and periodically while you are taking nilotinib.To decrease the risk of this effect, do not eat for 2 hours before or 1 hour after taking your dose. Other drugs/foods may increase the risk of an irregular heartbeat. Before taking this drug, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. See also How to Use and Drug Interactions sections.

            USES: Nilotinib is used to treat a certain type of blood cancer (chronic myelogenous leukemia-CML). It works by slowing or stopping the growth of cancer cells.

            HOW TO USE: Read the Medication Guide provided by your pharmacist before you start using nilotinib and each time you get a refill. If you have any questions, consult your doctor or pharmacist.Take this medication by mouth on an empty stomach as directed by your doctor, usually twice daily (about 12 hours apart). Swallow the capsule whole with water. Do not open, break, or chew the capsules. Do not eat any food for at least 2 hours before or for 1 hour after taking your dose. Taking this medication with food can increase the amount of drug in your body and increase the risk of serious side effects. If unable to swallow the capsules, the capsules may be opened and the contents sprinkled in 1 teaspoon of applesauce. This mixture should be swallowed right away (within 15 minutes). Use only 1 teaspoon of applesauce. Do not sprinkle the contents onto other types of food.Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor or pharmacist says you may do so safely. Grapefruit can increase the chance of side effects with this medicine. Ask your doctor or pharmacist for more details.Drink plenty of fluids during treatment with this medication, unless otherwise directed by your doctor.If you are also taking an antacid, take it 2 hours before or after nilotinib. If you are also taking an H2 blocker (such as cimetidine, famotidine), take it 10 hours before or 2 hours after nilotinib.The dosage is based on your medical condition, response to treatment, laboratory tests, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products). Children's dosage is also based on body size.Do not increase your dose or take this medication more often than prescribed. Your condition will not improve any faster, and the risk of serious side effects may be increased.Since this drug can be absorbed through the skin and lungs, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the contents of the capsules.

            SIDE EFFECTS: See also Warning section.Nausea, vomiting, headache, tiredness, constipation, and diarrhea may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.People using this medication may have serious side effects. However, you have been prescribed this drug because your doctor has judged that the benefit to you is greater than the risk of side effects. Careful monitoring by your doctor may decrease your risk.This medication decreases bone marrow function, an effect that may lead to a low number of blood cells such as red cells, white cells, and platelets. This effect can cause anemia, decrease your body's ability to fight an infection, or cause easy bruising/bleeding. Tell your doctor right away if you develop any of the following serious symptoms: severe tiredness, pale skin, signs of infection (such as sore throat that doesn't go away, fever, chills), easy bruising/bleeding (such as bloody/black stool, bloody/pink urine).Nilotinib sometimes causes side effects due to the rapid destruction of cancer cells (tumor lysis syndrome). To lower your risk, your doctor may add a medication and tell you to drink plenty of fluids. Tell your doctor right away if you have symptoms such as: low back/side pain (flank pain), signs of kidney problems (such as painful urination, change in the amount of urine), muscle spasms/weakness.Tell your doctor right away if you have any serious side effects, including: severe stomach/abdominal pain, toe/joint pain, swelling hands/ankles/feet, unusual/rapid weight gain, symptoms of high blood sugar (such as increased thirst/urination), signs of liver disease (such as nausea/vomiting that doesn't stop, stomach/abdominal pain, yellowing eyes/skin, dark urine).Get medical help right away if you have any very serious side effects, including: fast/pounding/irregular heartbeat, severe dizziness, fainting, seizures, signs of a heart attack (such as chest/jaw/left arm pain, shortness of breath, unusual sweating), signs of a stroke (such as weakness on one side of the body, trouble speaking, sudden vision changes, confusion), signs of bleeding in the brain (such as sudden severe headache, sudden vision changes, confusion, loss of consciousness), signs of blood circulation disease (such as numbness/pain in the legs, leg pain with physical activity, decrease in walking distance).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

            PRECAUTIONS: Before taking nilotinib, tell your doctor or pharmacist if you are allergic to it; or to lactose/galactose; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, pancreatitis, heart disease (such as coronary artery disease, chest pain, heart attack), high blood pressure, high cholesterol, diabetes, stroke (including "mini-strokes" or transient ischemic attacks), blood circulation disease (peripheral arterial disease), blood vessel disease (hardening of the arteries/atherosclerosis), stomach surgery (such as gastrectomy).Nilotinib may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can rarely cause serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that need medical attention right away.The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may cause QT prolongation. Before using nilotinib, tell your doctor or pharmacist of all the drugs you take and if you have any of the following conditions: certain heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/"water pills") or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using nilotinib safely.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Nilotinib can make you more likely to get infections or may worsen any current infections. Avoid contact with people who have infections that may spread to others (such as chickenpox, measles, flu). Consult your doctor if you have been exposed to an infection or for more details.Tell your health care professional that you are using nilotinib before having any immunizations/vaccinations. Avoid contact with people who have recently received live vaccines (such as flu vaccine inhaled through the nose).To lower the chance of getting cut, bruised, or injured, use caution with sharp objects like razors and nail cutters, and avoid activities such as contact sports.Children may be more sensitive to the side effects of this drug, especially liver disease, and slowed growth and development. Consult the doctor or pharmacist for more details. See the doctor regularly so your child's liver function, height, weight, and development can be checked.Older adults may be more sensitive to the side effects of this drug, especially QT prolongation (see above).Tell your doctor if you are pregnant or plan to become pregnant. You should not become pregnant while using nilotinib. Nilotinib may harm an unborn baby. Ask about reliable forms of birth control while using this medication and for 14 days after stopping treatment. If you become pregnant, talk to your doctor right away about the risks and benefits of this medication.It is not known whether this drug passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this drug and for 14 days after stopping treatment is not recommended. Consult your doctor before breast-feeding.

            DRUG INTERACTIONS: See also How to Use.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: antacids, flibanserin, H2 blockers (such as cimetidine/famotidine), proton pump inhibitors (such as omeprazole).Other medications can affect the removal of nilotinib from your body, which may affect how nilotinib works. Examples include azole antifungals (such as itraconazole, ketoconazole), macrolide antibiotics (such as clarithromycin), rifamycins (such as rifabutin), ritonavir, St. John's wort, drugs used to treat seizures (such as carbamazepine, phenytoin), among others.Many drugs besides nilotinib may affect the heart rhythm (QT prolongation), including amiodarone, dofetilide, pimozide, procainamide, quinidine, sotalol, macrolide antibiotics (such as erythromycin), among others.

            OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

            NOTES: Do not share this medication with others.Lab and/or medical tests (such as growth and development checks for children, complete blood count, EKG, electrolyte levels, liver function, lipase levels, uric acid level, cholesterol and blood sugar levels) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

            MISSED DOSE: If you miss a dose, take it as soon as you remember, but do not take if it is less than 2 hours before or 1 hour after a meal. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

            STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

            MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).

            Information last revised September 2022. Copyright(c) 2022 First Databank, Inc.

            IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

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            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.